Affiliation:
1. Department of Microbiology, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543-4000.
Abstract
The new antiviral nucleoside SQ 34,514 [(1R-1 alpha, 2 beta, 3 alpha)-2-amino-9- [2,3-bis(hydroxymethyl)cyclobutyl]-6H-purin-6-one], the active R isomer of racemic SQ 33,054 (cyclobut-G), was evaluated for efficacy in the treatment of herpesvirus infections in mice. SQ 34,514 was orally efficacious in a herpes simplex virus type 1 (HSV-1) systemic infection, an intracerebral HSV-2 infection, a vaginally induced HSV-2 infection in ovariectomized mice, and in a systemic murine cytomegalovirus infection. SQ 34,514 compared favorably with acyclovir and ganciclovir in the treatment of these experimental infections. In mice, SQ 34,514 had an oral bioavailability of 80% based on urinary excretion. SQ 34,514 may have potential value in the therapy of HSV and cytomegalovirus infections in humans.
Publisher
American Society for Microbiology
Subject
Infectious Diseases,Pharmacology (medical),Pharmacology
Reference23 articles.
1. Synthesis and antiviral activity of enantiomeric forms of cyclobutyl nucleoside analogues;Bisacchi G. S.;J. Med. Chem.,1991
2. Braitman A. J. M. Clark A. V. Tuomari J. S. Lynch B. McGeever-Rubin D. P. Bonner and A. K. Field. 1989. Efficacy of SQ 33 054 in herpes virus infections in mice. Program Abstr. 29th Intersci. Conf. Antimicrob. Agents Chemother. abstr. 1332.
3. Cunliffe-Beamer T. L. 1983. Biomethodology and surgical techniques p. 401-437. In H. L. Foster J. D. Small and J. G. Fox (ed.) The mouse in biomedical research vol. III. Normative biology immunology and husbandry. Academic Press Inc. New York.
4. Comparative efficacy of antiherpes drugs in different cell lines;De Clercq E.;Antimicrob. Agents Chemother.,1982
5. The disposition of acyclovir in different species;de Miranda P.;J. Pharmacol. Exp. Ther.,1981
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